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Activators and Inhibitors of Protein Kinase C (PKC): Their Applications in Clinical Trials
Protein kinase C (PKC), a family of phospholipid-dependent serine/threonine kinase, is classed into three subfamilies based on their structural and activation characteristics: conventional or classic PKC isozymes (cPKCs; α, βI, βII, and γ), novel or non-classic PKC isozymes (nPKCs; δ, ε, η, and θ),...
Autores principales: | , , , , |
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Formato: | Online Artículo Texto |
Lenguaje: | English |
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MDPI
2021
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Materias: | |
Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8621927/ https://www.ncbi.nlm.nih.gov/pubmed/34834162 http://dx.doi.org/10.3390/pharmaceutics13111748 |
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author | Kawano, Takahito Inokuchi, Junichi Eto, Masatoshi Murata, Masaharu Kang, Jeong-Hun |
author_facet | Kawano, Takahito Inokuchi, Junichi Eto, Masatoshi Murata, Masaharu Kang, Jeong-Hun |
author_sort | Kawano, Takahito |
collection | PubMed |
description | Protein kinase C (PKC), a family of phospholipid-dependent serine/threonine kinase, is classed into three subfamilies based on their structural and activation characteristics: conventional or classic PKC isozymes (cPKCs; α, βI, βII, and γ), novel or non-classic PKC isozymes (nPKCs; δ, ε, η, and θ), and atypical PKC isozymes (aPKCs; ζ, ι, and λ). PKC inhibitors and activators are used to understand PKC-mediated intracellular signaling pathways and for the diagnosis and treatment of various PKC-associated diseases, such as cancers, neurological diseases, cardiovascular diseases, and infections. Many clinical trials of PKC inhibitors in cancers showed no significant clinical benefits, meaning that there is a limitation to design a cancer therapeutic strategy targeting PKC alone. This review will focus on the activators and inhibitors of PKC and their applications in clinical trials. |
format | Online Article Text |
id | pubmed-8621927 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2021 |
publisher | MDPI |
record_format | MEDLINE/PubMed |
spelling | pubmed-86219272021-11-27 Activators and Inhibitors of Protein Kinase C (PKC): Their Applications in Clinical Trials Kawano, Takahito Inokuchi, Junichi Eto, Masatoshi Murata, Masaharu Kang, Jeong-Hun Pharmaceutics Review Protein kinase C (PKC), a family of phospholipid-dependent serine/threonine kinase, is classed into three subfamilies based on their structural and activation characteristics: conventional or classic PKC isozymes (cPKCs; α, βI, βII, and γ), novel or non-classic PKC isozymes (nPKCs; δ, ε, η, and θ), and atypical PKC isozymes (aPKCs; ζ, ι, and λ). PKC inhibitors and activators are used to understand PKC-mediated intracellular signaling pathways and for the diagnosis and treatment of various PKC-associated diseases, such as cancers, neurological diseases, cardiovascular diseases, and infections. Many clinical trials of PKC inhibitors in cancers showed no significant clinical benefits, meaning that there is a limitation to design a cancer therapeutic strategy targeting PKC alone. This review will focus on the activators and inhibitors of PKC and their applications in clinical trials. MDPI 2021-10-20 /pmc/articles/PMC8621927/ /pubmed/34834162 http://dx.doi.org/10.3390/pharmaceutics13111748 Text en © 2021 by the authors. https://creativecommons.org/licenses/by/4.0/Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (https://creativecommons.org/licenses/by/4.0/). |
spellingShingle | Review Kawano, Takahito Inokuchi, Junichi Eto, Masatoshi Murata, Masaharu Kang, Jeong-Hun Activators and Inhibitors of Protein Kinase C (PKC): Their Applications in Clinical Trials |
title | Activators and Inhibitors of Protein Kinase C (PKC): Their Applications in Clinical Trials |
title_full | Activators and Inhibitors of Protein Kinase C (PKC): Their Applications in Clinical Trials |
title_fullStr | Activators and Inhibitors of Protein Kinase C (PKC): Their Applications in Clinical Trials |
title_full_unstemmed | Activators and Inhibitors of Protein Kinase C (PKC): Their Applications in Clinical Trials |
title_short | Activators and Inhibitors of Protein Kinase C (PKC): Their Applications in Clinical Trials |
title_sort | activators and inhibitors of protein kinase c (pkc): their applications in clinical trials |
topic | Review |
url | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8621927/ https://www.ncbi.nlm.nih.gov/pubmed/34834162 http://dx.doi.org/10.3390/pharmaceutics13111748 |
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